SG175940A1 - Dihydropyrimidinones for use as bace2 inhibitors - Google Patents

Dihydropyrimidinones for use as bace2 inhibitors

Info

Publication number
SG175940A1
SG175940A1 SG2011082062A SG2011082062A SG175940A1 SG 175940 A1 SG175940 A1 SG 175940A1 SG 2011082062 A SG2011082062 A SG 2011082062A SG 2011082062 A SG2011082062 A SG 2011082062A SG 175940 A1 SG175940 A1 SG 175940A1
Authority
SG
Singapore
Prior art keywords
dihydropyrimidinones
use
bace2 inhibitors
bace2
inhibitors
Prior art date
Application number
SG2011082062A
Inventor
David Banner
Hans Hilpert
Roland Humm
Harald Mauser
Alexander V Mayweg
Fabienne Ricklin
Mark Rogers-Evans
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to EP09159740 priority Critical
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Priority to PCT/EP2010/056055 priority patent/WO2010128058A1/en
Publication of SG175940A1 publication Critical patent/SG175940A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

Abstract

This invention relates to dihydropyrimidinones of the formula (I), wherein X and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
SG2011082062A 2009-05-08 2010-05-05 Dihydropyrimidinones for use as bace2 inhibitors SG175940A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP09159740 2009-05-08
PCT/EP2010/056055 WO2010128058A1 (en) 2009-05-08 2010-05-05 Dihydropyrimidinones for use as bace2 inhibitors

Publications (1)

Publication Number Publication Date
SG175940A1 true SG175940A1 (en) 2011-12-29

Family

ID=42394975

Family Applications (1)

Application Number Title Priority Date Filing Date
SG2011082062A SG175940A1 (en) 2009-05-08 2010-05-05 Dihydropyrimidinones for use as bace2 inhibitors

Country Status (14)

Country Link
US (1) US8461160B2 (en)
EP (1) EP2427437A1 (en)
JP (1) JP5479575B2 (en)
KR (1) KR101372007B1 (en)
CN (1) CN102421760A (en)
AR (1) AR076754A1 (en)
AU (1) AU2010244470A1 (en)
BR (1) BRPI1014708A2 (en)
CA (1) CA2760343A1 (en)
IL (1) IL216145D0 (en)
MX (1) MX2011011854A (en)
SG (1) SG175940A1 (en)
TW (1) TW201043612A (en)
WO (1) WO2010128058A1 (en)

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EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
AR077328A1 (en) 2009-07-24 2011-08-17 Novartis Ag Oxazine derivatives and their use in treating neurological disorders
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MX2012006491A (en) 2009-12-11 2012-07-03 Shionogi & Co Oxazine derivative.
US8815881B2 (en) * 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co Fused aminodihydropyrimidine derivative
CN103261199A (en) 2010-10-29 2013-08-21 盐野义制药株式会社 Naphthyridine derivative
US8957083B2 (en) 2010-11-23 2015-02-17 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
KR101569260B1 (en) 2011-01-13 2015-11-13 노파르티스 아게 Novel heterocyclic derivatives and their use in the treatment of neurological disorders
US20140128385A1 (en) * 2011-01-13 2014-05-08 Novartis Ag Bace-2 inhibitors for the treatment of metabolic disorders
US9242943B2 (en) 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
WO2012109165A1 (en) 2011-02-07 2012-08-16 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
US8404680B2 (en) 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
US8962859B2 (en) 2011-02-15 2015-02-24 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
US9067924B2 (en) * 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
US8748418B2 (en) * 2011-03-18 2014-06-10 Hoffmann-La Roche Inc. 1,4-oxazepines as BACE1 and/or BACE2 inhibitors
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
CA2832473A1 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions, and their use
CN103608345A (en) 2011-04-26 2014-02-26 盐野义制药株式会社 Oxazine derivative and BACE 1 inhibitor containing same
CN103649082A (en) 2011-04-26 2014-03-19 盐野义制药株式会社 Pyridine derivative and bace-1 inhibitor containing same
US9079919B2 (en) * 2011-05-27 2015-07-14 Hoffmann-La Roche Inc. Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors
CN103874496A (en) 2011-08-22 2014-06-18 默沙东公司 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
UY34278A (en) * 2011-08-25 2013-04-05 Novartis Ag Oxazine novel derivatives and their use in the treatment of diseases
JP2014526560A (en) 2011-09-21 2014-10-06 アムジエン・インコーポレーテツド Aminooxazine and aminodihydrothiazine compounds as .BETA.-secretase modulators and methods of use
UA113538C2 (en) * 2012-01-26 2017-02-10 Ftormetil-5,6-digіdro-4h- [1,3] oxazines
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
AU2013265376B2 (en) * 2012-05-24 2017-07-20 F. Hoffmann-La Roche Ag 5-amino[1,4]thiazines as BACE 1 inhibitors
KR20150023536A (en) * 2012-05-30 2015-03-05 코멘티스, 인코포레이티드 Chromane compounds
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CN104870000A (en) 2012-12-20 2015-08-26 默沙东公司 C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors
US9489013B2 (en) 2012-12-20 2016-11-08 Merck Sharp & Dohme Corp. C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use
US9580396B2 (en) 2012-12-21 2017-02-28 Merck Sharp & Dohme Corp. C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
MX2015011313A (en) 2013-03-01 2015-12-03 Amgen Inc Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use.
AU2014225604B2 (en) 2013-03-08 2018-05-17 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN103387545A (en) * 2013-08-10 2013-11-13 谢永荣 Method for preparing dihydropyrimidinone sulphonic derivative
CA2957544A1 (en) 2014-08-08 2016-02-11 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
KR20170129745A (en) 2015-03-20 2017-11-27 에프. 호프만-라 로슈 아게 BACE1 inhibitor

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JP2008503459A (en) 2004-06-16 2008-02-07 ワイス Amino-5,5-diphenyl imidazolone derivatives for inhibiting β- secretase
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Also Published As

Publication number Publication date
CA2760343A1 (en) 2010-11-11
US8461160B2 (en) 2013-06-11
AU2010244470A1 (en) 2011-12-01
KR101372007B1 (en) 2014-03-07
US20100286158A1 (en) 2010-11-11
MX2011011854A (en) 2011-12-06
AR076754A1 (en) 2011-07-06
EP2427437A1 (en) 2012-03-14
BRPI1014708A2 (en) 2016-04-12
KR20120061069A (en) 2012-06-12
TW201043612A (en) 2010-12-16
JP2012526076A (en) 2012-10-25
JP5479575B2 (en) 2014-04-23
CN102421760A (en) 2012-04-18
IL216145D0 (en) 2012-01-31
WO2010128058A1 (en) 2010-11-11

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